Home Neuronal Signaling Adrenergic Receptor antagonist Terazosin HCl Dihydrate

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Terazosin HCl Dihydrate Adrenergic Receptor antagonist

Cat.No.S2059

Terazosin HCl is a selective α1-adrenoceptor antagonist, used for treatment of symptoms of an enlarged prostate (BPH).
Terazosin HCl Dihydrate Adrenergic Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 459.92

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Quality Control

Batch: S205901 DMSO]26 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.97%
99.97

Chemical Information, Storage & Stability

Molecular Weight 459.92 Formula

C19H25N5O4.HCl.2H2O

 Storage (From the date of receipt)
CAS No. 70024-40-7 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles COC1=C(C=C2C(=C1)C(=NC(=N2)N3CCN(CC3)C(=O)C4CCCO4)N)OC.O.O.Cl

Solubility

In vitro
Batch:

DMSO : 26 mg/mL ( (56.53 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

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In vivo
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Mechanism of Action

Targets/IC50/Ki
α-adrenergic receptor [1]
In vitro
Terazosin results in a significant loss of cell viability, via induction of apoptosis in a dose-dependent manner in prostate cancer cells. Terazosin suppresses prostate growth potentially via α 1-adrenoceptor-independent actions gains further support from another study documenting that Doxazosin inhibits proliferation of human vascular smooth muscle cells independently of an antagonistic effect on α1-adrenoceptor. [1] Terazosin blocks HERG currents in Xenopus oocytes with IC50 of 113.2 mM, while Terazosin blocks HERG channel inhibition in human HEK 293 cells with IC50 of 17.7 mM. [2] Terazosin or genistein treatment inhibits the growth of DU-145 cells in a dose-dependent manner, whereas has no effect on normal prostate epithelial cells. Terazosin results in the genistein-induced arrest of DU-145 cells in G2/M phase being overridden and an increase in apoptotic cells, as evidenced by procaspase-3 activation and PARP cleavage. [3] Terazosin induces cytotoxicity in PC-3 and human benign prostatic cells with an IC50 of more than 100 mM. [4]
In vivo
Terazosin significantly inhibits vascular endothelial growth factor induced angiogenesis in nude mice with an IC50 of 7.9 mM, showing that it has a more potent anti-angiogenic than cytotoxic effect. Terazosin also effectively inhibits vascular endothelial growth factor induced proliferation and tube formation in cultured human umbilical vein endothelial cells (IC50 9.9 and 6.8 mM, respectively). [4]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04760860 Not yet recruiting
Dementia With Lewy Bodies
Qiang Zhang|University of Iowa
 October 2024 Phase 1|Phase 2
NCT04551040 Active not recruiting
Healthy
University of Iowa|Michael J. Fox Foundation for Parkinson''s Research
 March 26 2021 Phase 1
NCT04386317 Recruiting
REM Sleep Behavior Disorder|Pre-motor Parkinson''s Disease|Symptomatic Parkinson Disease
Cedars-Sinai Medical Center
 November 1 2020 Phase 2
NCT00449683 Completed
Hyperhidrosis
Thomas Jefferson University|National Alliance for Research on Schizophrenia and Depression
 March 2007 Phase 4
NCT00237510 Completed
Antidepressant Induced Excessive Sweating
Thomas Jefferson University
 May 2005 Not Applicable
NCT02244333 Completed
Prostatic Hyperplasia
Boehringer Ingelheim
 February 2004 --

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